Sodium-glucose cotransporter 2 (SGLT2) (SGLT2)

The sodium-glucose cotransporter 2 (SGLT2), encoded by the SLC5A2 gene on chromosome 16p11.2, is a membrane protein primarily expressed in the early proximal tubule of the kidney, where it mediates sodium-dependent reabsorption of 80-90% of filtered glucose. By coupling glucose uptake with sodium influx, SGLT2 plays a critical role in renal glucose homeostasis, preventing glucosuria under normal conditions. Dysregulation contributes to hyperglycemia in type 2 diabetes mellitus, while inhibition promotes glycosuria, lowering blood glucose independently of insulin. SGLT2 inhibitors like canagliflozin, dapagliflozin, and empagliflozin demonstrate cardiovascular and renal protective effects, reducing heart failure hospitalization, cardiovascular death, and chronic kidney disease progression. Emerging evidence also links SGLT2 expression to early-stage lung adenocarcinoma, suggesting diagnostic and therapeutic potential via PET imaging and inhibitors. Overall, SGLT2 represents a validated therapeutic target with pleiotropic benefits beyond glycemic control.

Other names

sodium/glucose cotransporter 2solute carrier family 5 member 2SLC5A2low affinity sodium-glucose cotransporterlow affinity Na-dependent glucose transporter

Inhibition of sodium-glucose cotransport in proximal tubule, promoting urinary glucose excretion, reducing blood glucose levels